Autonomic Pharm & Kinetics Flashcards

1
Q

On the log enzyme kinetics graph, y-intercept is equal to?

A

1/Vmax

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2
Q

The lower the Km,

the _____ the affinity.

A

higher

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3
Q

On the log kinetics graph:
Competitive inhibitors cross each other competitively.
T/F

A

T

They all cross on 1/Vmax

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4
Q

On the log kinetics graph:
Noncompetitive inhibitors do not cross each other.
T/F

A

T

they have different Km’s

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5
Q

Vd = ?

A

amt of drug in body /

plasma drug concentration

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6
Q

t1/2 = ?

A

0.7 * Vd / clearanc

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7
Q

A drug infused at a constant rate reaches about 94% of steady state after x half-lives?

A

x = 4

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8
Q

Loading dose = ?

A

Cp * Vd/F

Cp = target plasma conc.
F = bioavailability: =1 per IV
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9
Q

Phase 1 metabolism involves?

yields?

A

reduction, oxidation, hydrolysis
cytochrome P450
yields slightly polar, still-active water-soluble metabolites
Geriatrics lost this first

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10
Q

Phase 2 metabolism involves?

yields?

A

acetylation, glucuronidation, sulfation, conjugation

yields very polar, inactive metabolites

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11
Q
Potency = ?
Efficacy = ?
A

Potency = amt needed for a given effect

Efficacy = maximal effect

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12
Q

Therapeutic index =

A

TD50 /
ED50

(median toxic dose /
median effective dose)

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13
Q

Skeletal Muscle.
N or M?
neurotransmitter?

A

N

ACh

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14
Q

PNS: Cardiac & Smooth Muscle, gland cells.
N or M?
neurotransmitter?

A

N——-M (2 neurons)

Ach Ach

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15
Q

All sympathetic @ ganglion.
N or M?
neurotransmitter?

A

N

ACh

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16
Q

Sympathetic 2nd neuron @ sweat glands:
N or M?
neurotransmitter?

A

M

ACh

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17
Q

Sympathetic @ cardiac and smooth muscle, gland cells, nerve terminals

neurotransmitter?

A

NE @ alpha or beta

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18
Q

Sympathetic at Renal vascular smooth muscle

receptor??

A

D1

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19
Q

Sympathetic @ adrenal medulla

N or M?
neurotransmitter?

A

N, ACh

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20
Q

G-protein-linked 2nd messengers:
a1 ->

G-prot class?
functions?

A

q

Inc’d vascular smooth muscle contraction

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21
Q

G-protein-linked 2nd messengers:

a2

A
i
Dec'd sympathetic outflow
Dec'd insulin release
Dec'd lipolysis
Inc'd platelet aggregation
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22
Q

G-protein-linked 2nd messengers:

B1

A
s
Inc'd HR, 
Inc'd contactility
Inc'd renin release
Inc'd lipolysis
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23
Q

G-protein-linked 2nd messengers:

B2

A
s
vasodilation, bronchodilation
Inc'd HR, contractility, lipolysis, insulin release, aqueous humor production
Dec'd uterine tone (tocolysis)
Ciliary muscle relaxation
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24
Q

G-protein-linked 2nd messengers:

M1

A

q

CNS

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25
Q

G-protein-linked 2nd messengers:

M2

A

i

Dec’d HR & contractility of atria

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26
Q

G-protein-linked 2nd messengers:

M3

A

q
Inc’d exocrine gland secretions, gut peristalsis, bladder contraction, bronchoconstriction, pupillary sphincter muscle (miosis) & ciliary muscle contraction (accommodation)

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27
Q

G-protein-linked 2nd messengers:

D1

A

s

relaxes renal vascular smooth muscle

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28
Q

G-protein-linked 2nd messengers:

D2

A

i

modulates transmitter release, esp in brain

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29
Q

G-protein-linked 2nd messengers:

H1

A
q
Inc'd nasal/bronchial mucus
bronchconstriction
pruritis
pain
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30
Q

G-protein-linked 2nd messengers:

H2

A

s

Inc’d gastic acid secretion

31
Q

G-protein-linked 2nd messengers:

V1

A

contracts vascular smooth muscle

32
Q

G-protein-linked 2nd messengers:

V2

A

Inc’d H20 permeability & reabsorption in the collective tubules

33
Q

H1, a1, V1, M1, M3

G-prot class?
cell signals?

A

Gq — Phoslipase C — PIP2 — DAG & IP3…

IP3 — inc Ca (smooth muscle contraction
DAG — PKC

34
Q

B1, B2, D1, H2, V2

G-prot class?
cell signals?

A

Gs — adenylcyclase — (converts ATP into cAMP)…

cAMP — PKA — 2 actions:

  1. inc’d Ca(2+) in heart
  2. inhibits myosin light chain kinase (smooth muscle)
35
Q

M2, a2, D2

A

Gi (inhibits) —X adenylcyclase — (converts ATP into cAMP)…

cAMP — PKA — 2 actions:

  1. inc’d Ca(2+) in heart
  2. inhibits myosin light chain kinase (smooth muscle)
36
Q

Guanethidine

A

decreases NE release

37
Q

Metyrosine

A

decreases DOPA formation from tyrosine

38
Q

Reserpine

A

inhibits DA uptake into secretory vesicles; inhibiting its release @ nerve junction

39
Q

Hemicholinium?

Vesamicol?

A

H: inhibits presynaptic choline reuptake

V: inhibits ACh loading into secretory vesicles

40
Q

Bethanechol

clin?
action?

A

cholinomimetic direct agonist

clin: postop & neurogenic ileus & urinary retention
action: activates Bowel & Bladder smooth muscle; resistant to AChE

41
Q

Carbachol

clin?
action?

A

Cholinomimetic direct agonist

clin: glaucoma, pupillary contraction, & release of intraocular pressure
act: contracts ciliary muscle of eye (open angle), pupillar sphincter (narrow angle); resistant to AChE

42
Q

Pilocarpine

A

cholinomimetic direct agonist

potent stimulator of sweat, tears, saliva

43
Q

Methacholine

A

cholinomimetic direct agonist
challenge test for dx of asthma
stimulates muscarinic receptors

44
Q

Neostigmine

A

cholinomimetic indirect agonist

clin: postop & neurogenic ileus & urinary retention, myasthenia gravis, reversal of nueromuscular junction blockade(postop)
act: inc’d endogenous ACh; no CNS penetration

45
Q

Pyridostigmine

A

cholinomimetic indirect agonist
myasthenia gravis, increases strength
act: inc’d endogenous ACh; no CNS penetrance

46
Q

Edrophonium

A

cholinomimetic indirect agonist
dx of Myasthenia G (extremely short acting)
act: inc’d endogenous ACh;

47
Q

Physostigmine

A

cholinomimetic indirect agonist
glaucoma (crosses BBB to CNS) and atropine OD
act: inc’d endogenous ACh;

48
Q

Echothiophate

A

cholinomimetic indirect agonist
glaucoma
act: inc’d endogenous ACh;

49
Q

Cholinesterase inhibitor poisoning symptoms:
antidote?

DUMBBELSS

A
Diarrhea
Urination
Miosis
Bronchospasm
Bradycardia
Excitation of skeletal muscle and CNS
Lacrimation
Sweating 
Salivation (also abd cramps)

ANTIDOTE: atropine (muscarinic antagonist) plus pralidoxime (chemical antagonist used to regenerate active cholinsterase)

50
Q

homatropine
tropicamide
atropine

A

Muscarinic antagonist (eye)

produces mydriasis & cycloplegia

51
Q

Benztropine

A

Muscarinic antagonist (CNS)

parkinson’s dz (2nd line)

52
Q

Scopolamine

A

Muscarinic antagonist (CNS)

motion sickness

53
Q

Ipratropium, Tiotropium

A

Muscarinic antagonist (respiratory)

Asthma, COPD

54
Q

Oxybutynin, Glycopyrrolate

A

O: Muscarinic antagonist (genitourinary)
Reduces urgency in mild cystitis and reduces bladder spasms

G: Muscarinic antagonist (GI, respiratory)
Parenteral: pre-op to reduce airway secretions
Oral: drooling, peptic ulcer

55
Q

Glaucoma
brimonide

mech?
tox?

A

mech: alpha agonist
_aqueous humor synth

SE: no pupillary or vision changes

56
Q

Glaucoma
betaxolol, timolol, carteolol

mech?
tox?

A

mech: beta-blocker
_aqueous humor secretion

SE: no pupillary or vision changes

57
Q

Glaucoma
Acetazolamide

mech?
tox?

A

mech: diuretic
_aqueous humor secretion via inhibition of carbonic anydrase

SE: no pupillary or vision changes

58
Q

Glaucoma
pilocarpine, carbachol, physostigmine, echothiophate

mech?
tox?

A

mech: cholinomimetic
_outflow of aqueous humor; contracts ciliary muscle –>
opens trabecular meshwork
use pilocarpine in emergencies as it is very effetive at opening canal of Schlemm

SE: miosis, cyclospasm

59
Q

Glaucoma
Latanoprost

mech?
tox?

A

mech: prostaglandin
_outflow of aqueous humor;

tox: darkens color of iris (browning)

60
Q

ATROPINE

uses?

A

Muscarinic antagonist

EYE: _pupil dilation, cycloplegia
AIRWAY: _secretions
Stomach: _acid secretion
Gut: _motility
Bladder: _urgency in cystitis
BLOCKS SLUD: 
Salivation
Lacrimation
Urination
Defecation
61
Q

ATROPINE

tox?

A

TOX:
_body temp; rapid pulse; dry mouth; dry, flushed skin; cycloplegia; constipation; disorientation

can cause acute angle-closure glaucoma in elderly, urinary retention in men w/prostatic hypertrophy, and hyperthermia in infants

62
Q

Hot as a…

A
Hot as a hare
Dry as a bone, 
red as a beet,
blind as a bat
mad as a hatter
63
Q

Hexamethonium

A

mech: nicotinic ACh receptor antagonist
clin: ganglionic blocker. Used in exp models to prevent vagal reflexz response to changes in BP–e.g. prevents reflex bradycardia caused by NE

64
Q

Sympathomimetic selectivity

Epi

A

__ __ __ __
low doses selective for __

uses: anaphylaxis, glaucoma(open angle), asthma, hypoTN

65
Q

Sympathomimetic selectivity

NE

A

__ __ > __
_SBP, DBP –> reflex bradycardia

clin:
hypoTN(but _renal perfusion)

66
Q

Sympathomimetic selectivity

Iso

A

__=__ > __ __
_SBP, DBP
_HR

clin: AV block (rare)

67
Q

Sympathomimetic selectivity

Dopa

A

D1=D2 > __ __ > __ __

clin:
shock(increases renal perfusion), HF

68
Q

Sympathomimetic selectivity

Dobu

A

__ __ __ __

69
Q

Phenoxybenzamine (irrev)

phentolamine (rev)

A

nonsel. _-blocker

clin: pheochromocytoma
tox: orthostatic HTN
reflex tachycardia

70
Q

Prazosin, terazosin, doxazosin

A

__ selective

clin: HTN, BPH
tox: 1st dose orthoHTN, dizziness, headache

71
Q

Mirtazapine

A

__ selective

clin: depression
tox: sedation, _serum chol, _appetite

72
Q

olol’s

clin & tox?

A
Beta-blockers
HTN: _CO, _renin secretion
Angina: _HR/contractility, resulting in _O2 use
MI: _mortality
SVT: _AV conduction velocity
CHF: slows progression of CHF
Glaucoma (timolol): _aq humor secretion

TOX: impotence, exacerabtion of asthma, CV adverse effects, CNS adverse effects

73
Q

olol’s

non selective & selective(A BEAM of b1 blockers)?

A

nonselective: propranolol, timolol, nadolol, pindolol (partial agonist), labetalol (partial agonist)
Beta1 selective: Acetbutolol (partial), betaxolol, Esmolol (short acting), Atenolol, Metroprolol